Based on the ligand selectivity in the receptor binding assay as seen in different tissues, the sigma receptor was found to consist of two subtypes, the sigma-1 and sigma-2 receptors. The incorrect early assumption that the sigma receptors would be members of the family of opioid receptors has been declined since the early 1990’s[1]. After many years of research, now it has been revealed that the sigma-1 receptor is a unique ligand-regulated molecular chaperone in the endoplasmic reticulum of cells[2]. Evidence was found that the most prominent action of sigma-1 receptors in biological systems is the regulation and modulation of voltage-regulated and ligand-gated ion channels, including Ca(2+)-, K(+)-, Na(+), Cl(-), and SK channels, and NMDA and IP3 receptors. Stimulation of the receptor by sigma-1 agonists causes inhibition of all above-mentioned voltage-gated ion channels, while on the other hand it potentiates ligand-gated channels[3]. In contrast, little is known to date of the sigma-2 receptor which is still to be cloned. Activation of the receptor seems to cause apoptosis[4].

[1] Rat liver and kidney contain high densities of sigma-1 and sigma-2 receptors: Characterization by ligand binding and photoaffinity labeling. S.B. Hellewell, A. Bruce, G. Feinstein, J. Orringer, W. Williams, W.D. Bowen. Eur. J. Pharmacol. 1994, 268, 9-18.
[2] The sigma-1 receptor chaperone as an inter-organelle signaling modulator. T.P. Su, T. Hayashi, T. Maurice, S. Buch, A.E. Ruoho. Trends Pharmacol. Sc. 2010, 31, 557-566.
[3] The pharmacology of sigma-1 receptors. T. Maurice, T.P. Su. Pharmacol. Ther. 2009, 124, 195-206.
[4] Sigma receptors: recent advances and new clinical potentials. W.D. Bowen. Pharm. Acta Helv. 2000, 74,  211-218.


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Axon ID Name Description From price
2919 4-IBP Selective sigma-1 (σ-1) receptor agonist €90.00
1215 BD 1047 dihydrobromide Sigma-1 antagonist €75.00
2088 BD 1063 dihydrochloride Selective sigma-1 (σ-1) receptor antagonist €75.00
1272 PB28 dihydrochloride Sigma-2 agonist €85.00
3063 PRE-084 hydrochloride Highly selective sigma-1 (σ-1) agonist €75.00
3859 Roluperidone Sigma-2 and 5-HT2A receptor antagonist €120.00
1767 SA 4503 Sigma-1 receptor antagonist €120.00

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